SG11201805202VA - 6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE DOPAMINE D3 LIGANDS - Google Patents

6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE DOPAMINE D3 LIGANDS

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Publication number
SG11201805202VA
SG11201805202VA SG11201805202VA SG11201805202VA SG11201805202VA SG 11201805202V A SG11201805202V A SG 11201805202VA SG 11201805202V A SG11201805202V A SG 11201805202VA SG 11201805202V A SG11201805202V A SG 11201805202VA SG 11201805202V A SG11201805202V A SG 11201805202VA
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SG
Singapore
Prior art keywords
massachusetts
street
international
road
rule
Prior art date
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SG11201805202VA
Inventor
Thomas Allen Chappie
Jaclyn Louise Henderson
Joseph Michael Young
Travis T Wager
Bethany Lyn Kormos
Nandini Chaturbhai Patel
Simone Sciabola
Jamison Bryce Tuttle
Patrick Robert Verhoest
Joseph Walter Tucker
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Pfizer
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Publication of SG11201805202VA publication Critical patent/SG11201805202VA/en

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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 111111110111101110101011111010111110111011101110111011101111101111101111011111 International Bureau 0.. .... .. (10) International Publication Number ..... ..or::,„, (43) International Publication Date WO 2017/122116 Al 20 July 2017 (20.07.2017) WIPO I PCT (51) International Patent Classification: (74) Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd C07D 471/04 (2006.01) A61P 3/04 (2006.01) Street, MS 235/9/S20, New York, New York 10017 (US). A61K 31/55 (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of national protection available): AE, AG, AL, AM, PCT/IB2017/050094 AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (22) International Filing Date: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 9 January 2017 (09.01.2017) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (25) Filing Language: English KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (26) Publication Language: English NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (30) Priority Data: RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 62/279,037 15 January 2016 (15.01.2016) US TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, New York, New York 10017 (US). (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (72) Inventors: CHAPPIE, Thomas Allen; 59 Hemlock Hill GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Road, Carlisle, Massachusetts 01741 (US). HENDER- TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, SON, Jaclyn Louise; 36 Highland Avenue, Apt. 54, Cam- TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, bridge, Massachusetts 02139 (US). YOUNG, Joseph Mi- DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, — chael; 20156 Stanton Avenue, #36, Castro Valley, Califor- LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, — nia 94546 (US). WAGER, Travis T.; _ 465 Washington SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Street, Apt., 6, Brookline, Massachusetts 02446 (US). GW, KM, ML, MR, NE, SN, TD, TG). Street, #3, KORMOS, Bethany Lyn; 46 Quincy Nandini Declarations under Rule 4.17: = Somerville, Massachusetts 02143 (US). PATEL, Massachusetts — as to the identity of the inventor (Rule 4.17(1)) Chaturbhai; 34 Mary Ellen Road, Waban, 02468 (US). SCIABOLA, Simone; 109 River Street, Cam- as to applicant's entitlement to apply for and be granted a Jamison patent (Rule 4.17(11)) Massachusetts bridge, Massachusetts 02139 (US). TUTTLE, = — Bryce; 24 Amherst Road, Marblehead, 23 Calvin — as to the applicant's entitlement to claim the priority of the = 01945 (US). VERHOEST, Patrick Robert; TUCKER, earlier application (Rule 4.17(iii)) Road, Newton, Massachusetts 02460 (US). = Joseph Walter; 25 Dart Street, New London, Connecticut Published: 06320 (US). — with international search report (Art. 21(3)) = = = = = DOPAMINE D3 LIGANDS — (54) Title: 6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE = (R 2 ) a R 3 .,, ,............7 „ K l r . - - 4— ... ,. ,..., 1 (I) N —R 1 0 0 Il % / R ,tD 5 S N , ..,, , ..,„,\" •••••,, 1-1 A 1-1 ei ei ,-1 N R 4 L ---- (57) : The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the ::::) variables R I , R 2 , R 3 , R, R 4 5 , a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; N and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders includ - 0 ing, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive ,-t impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual dis - .,- orders and depression.
SG11201805202VA 2016-01-15 2017-01-09 6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE DOPAMINE D3 LIGANDS SG11201805202VA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662279037P 2016-01-15 2016-01-15
PCT/IB2017/050094 WO2017122116A1 (en) 2016-01-15 2017-01-09 6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE DOPAMINE D3 LIGANDS

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SG11201805202VA true SG11201805202VA (en) 2018-07-30

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Country Status (16)

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US (2) US10590128B2 (en)
EP (1) EP3402796B1 (en)
JP (1) JP6929857B2 (en)
KR (1) KR102206321B1 (en)
CN (1) CN108884093B (en)
AU (1) AU2017208119B2 (en)
BR (1) BR112018013955B1 (en)
CA (1) CA3011201C (en)
ES (1) ES2837018T3 (en)
IL (1) IL260298B (en)
MX (1) MX2018008653A (en)
RU (1) RU2712455C1 (en)
SG (1) SG11201805202VA (en)
TW (1) TWI633104B (en)
WO (1) WO2017122116A1 (en)
ZA (1) ZA201803776B (en)

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WO2017122116A1 (en) 2017-07-20
BR112018013955A2 (en) 2018-12-11
CN108884093A (en) 2018-11-23
CA3011201C (en) 2020-09-22
CA3011201A1 (en) 2017-07-20
AU2017208119B2 (en) 2019-11-07
TWI633104B (en) 2018-08-21
ES2837018T3 (en) 2021-06-29
CN108884093B (en) 2021-07-09
AU2017208119A1 (en) 2018-06-28
US20200157098A1 (en) 2020-05-21
US10590128B2 (en) 2020-03-17
US11390623B2 (en) 2022-07-19
RU2712455C1 (en) 2020-01-29
EP3402796A1 (en) 2018-11-21
JP2019501930A (en) 2019-01-24
KR102206321B1 (en) 2021-01-21
BR112018013955B1 (en) 2024-01-16
US20190047997A1 (en) 2019-02-14
MX2018008653A (en) 2018-12-10
KR20180100432A (en) 2018-09-10
ZA201803776B (en) 2020-09-30
TW201736367A (en) 2017-10-16
EP3402796B1 (en) 2020-11-18
JP6929857B2 (en) 2021-09-01
IL260298A (en) 2018-08-30
IL260298B (en) 2021-07-29

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